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Pronunciation:

(es TA zoe lam)

U.S. Brand Names:

ProSom®

Generic Available:

Yes

Use:

Short-term management of insomnia

Restrictions:

C-IV

Pregnancy Risk Factor:

Lactation:

Enters breast milk/contraindicated

Contraindications:

Hypersensitivity to estazolam or any component of the formulation (cross-sensitivity with other benzodiazepines may exist); pregnancy

Note: Manufacturer states concurrent therapy with itraconazole or ketoconazole is contraindicated.

Warnings/Precautions:

As a hypnotic, should be used only after evaluation of potential causes of sleep disturbance. Failure of sleep disturbance to resolve after 7-10 days may indicate psychiatric or medical illness. Use is not recommended in patients with depressive disorders or psychoses. Avoid use in patients with sleep apnea. Use with caution in patients receiving concurrent CYP3A4 inhibitors, particularly when these agents are added to therapy. Use with caution in elderly or debilitated patients, patients with hepatic disease (including alcoholics), renal impairment, respiratory disease, impaired gag reflex, or obese patients.

Causes CNS depression (dose-related) which may impair physical and mental capabilities. Use with caution in patients receiving other CNS depressants or psychoactive agents. Benzodiazepines have been associated with falls and traumatic injury and should be used with extreme caution in patients who are at risk of these events (especially the elderly). May cause physical or psychological dependence - use with caution in patients with a history of drug dependence.

Benzodiazepines have been associated with anterograde amnesia. Paradoxical reactions, including hyperactive or aggressive behavior, have been reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients. Does not have analgesic, antidepressant, or antipsychotic properties.

Adverse Reactions:

>10%:

Central nervous system: Somnolence

Neuromuscular & skeletal: Weakness

1% to 10%:

Cardiovascular: Flushing, palpitation

Central nervous system: Anxiety, confusion, dizziness, hypokinesia, abnormal coordination, hangover effect, agitation, amnesia, apathy, emotional lability, euphoria, hostility, seizure, sleep disorder, stupor, twitch

Dermatologic: Dermatitis, pruritus, rash, urticaria

Gastrointestinal: Xerostomia, constipation, decreased appetite, flatulence, gastritis, increased appetite, perverse taste

Genitourinary: Frequent urination, menstrual cramps, urinary hesitancy, urinary frequency, vaginal discharge/itching

Neuromuscular & skeletal: Paresthesia

Ocular: Photophobia, eye pain, eye swelling

Respiratory: Cough, dyspnea, asthma, rhinitis, sinusitis

Miscellaneous: Diaphoresis

<1%: Allergic reactions, chills, drug dependence, fever, muscle spasm, myalgia, neck pain

Overdosage/Toxicology:

Symptoms of overdose include respiratory depression, hypoactive reflexes, unsteady gait, and hypotension. Treatment for benzodiazepine overdose is supportive. Flumazenil has been shown to selectively block the binding of benzodiazepines to CNS receptors, resulting in a reversal of benzodiazepine-induced sedation; however, its use may not reverse respiratory depression.

Drug Interactions:

Substrate of CYP3A4 (minor)

CNS depressants: Sedative effects and/or respiratory depression may be additive with CNS depressants; includes ethanol, barbiturates, narcotic analgesics, and other sedative agents; monitor for increased effect

Itraconazole, ketoconazole: Concurrent use is contraindicated (per manufacturer); however, estazolam is a minor CYP3A4 substrate and an effect has not been documented in clinical studies.

Levodopa: Therapeutic effects may be diminished in some patients following the addition of a benzodiazepine; limited/inconsistent data

Oral contraceptives: May decrease the clearance of some benzodiazepines (those which undergo oxidative metabolism); monitor for increased benzodiazepine effect

Theophylline: May partially antagonize some of the effects of benzodiazepines; monitor for decreased response; may require higher doses for sedation

Ethanol/Nutrition/Herb Interactions:

Ethanol: Avoid ethanol (may increase CNS depression).

Food: Serum levels and/or toxicity may be increased by grapefruit juice.

Mechanism of Action:

Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization.

Pharmacodynamics/Kinetics:

Onset of action: ~1 hour

Duration: Variable

Metabolism: Extensively hepatic

Half-life elimination: 10-24 hours (no significant changes in elderly)

Time to peak, serum: 0.5-1.6 hours

Excretion: Urine (<5% as unchanged drug)

Dosage:

Adults: Oral: 1 mg at bedtime, some patients may require 2 mg; start at doses of 0.5 mg in debilitated or small elderly patients

Dosing adjustment in hepatic impairment: May be necessary

Monitoring Parameters:

Respiratory and cardiovascular status

Patient Education:

Use exactly as directed; do not increase dose or frequency or discontinue without consulting prescriber. Drug may cause physical and/or psychological dependence. While using this medication, do not use alcohol or other prescription or OTC medications (especially, pain medications, sedatives, antihistamines, or hypnotics) without consulting prescriber. Maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake. You may experience drowsiness, dizziness, or blurred vision (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or GI upset (take with water or milk). Report CNS changes (confusion, depression, increased sedation, excitation, headache, abnormal thinking, insomnia, or nightmares); altered voiding patterns or blood in urine; respiratory difficulty, chest pain, or palpitations; altered gait pattern; or ineffectiveness of medication. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not get pregnant during therapy or for 1 month following therapy. Consult prescriber for instruction on appropriate contraceptive measures. This drug may cause severe fetal defects. Do not breast-feed.

Nursing Implications:

Provide safety measures (ie, side rails, night light, and call button); remove smoking materials from area; supervise ambulation; avoid abrupt discontinuance in patients with prolonged therapy or seizure disorders

Additional Information:

Abrupt discontinuation after sustained use (generally >10 days) may cause withdrawal symptoms.

Anesthesia and Critical Care Concerns/Other Considerations:

Abrupt discontinuation after sustained use (generally >10 days) may cause withdrawal symptoms.

Dental Health: Effects on Dental Treatment:

Key adverse event(s) related to dental treatment: Significant xerostomia (normal salivary flow resumes upon discontinuation).

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Dosage Forms:

Tablet: 1 mg, 2 mg

International Brand Names:

Domnamid® (DK); Esilgan® (HK, ID, IT); Estazolam® (PL); Eurodin® (JP); Kainever® (PT); Noctal® (BR); Nuctalon® (FR); Tasedan® (MX)

References

Busto U, Bendayan R, and Sellers EM, "Clinical Pharmacokinetics of Nonopiate Abuse Drugs,"Clin Pharmacokinet, 1989, 16(1):1-26.

Mokhlesi B, Leikin JB, Murray P, et al, "Adult Toxicology in Critical Care: Part II: Specific Poisonings,"Chest, 2003, 123(3):897-922.

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